Biology:Hydroxycarboxylic acid receptor 1
 Generic protein structure example |
Hydroxycarboxylic acid receptor 1 (HCA1), formerly known as G protein-coupled receptor 81 (GPR81), is a protein that in humans is encoded by the HCAR1 gene.[1][2] HCA1, like the other hydroxycarboxylic acid receptors HCA2 and HCA3, is a Gi/o-coupled G protein-coupled receptor (GPCR).[3][4] The primary endogenous agonist of HCA1 is lactic acid (and its conjugate base, lactate).[3][4] More recently, 3,5-dihydroxybenzoic acid has been reported to activate HCA1.[5]
Lactate was initially found to activate HCA1 on fat cells and thereby to inhibit these cells lipolysis i.e., break-down of their fats into free fatty acids and glycerol.[6][7] Subsequent studies have found that in addition to fat cells, HCA1 is expressed on cells in the brain, skeletal muscle, lymphoid tissue, uterus, kidney, liver, and pancreas as well as on immune cells such as macrophages and antigen-presenting cells. In the brain, HCA1 acts to dampen neuron excitation and may also function to promote neurogenesis (i.e., production of neurons from neural stem cells) and angiogenesis, i.e., formation of new blood vessels from pre-existing blood vessels). The functions of HCA1 in non-fat and non-neural tissues have not been fully defined but in many cases appear to involve promoting the survival of cells, including various types of cancer cells.[8]
References
- ↑ "Entrez Gene: GPR81 G protein-coupled receptor 81". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=27198.
- ↑ "Discovery and mapping of ten novel G protein-coupled receptor genes". Gene 275 (1): 83–91. September 2001. doi:10.1016/S0378-1119(01)00651-5. PMID 11574155.
- ↑ 3.0 3.1 "International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B)". Pharmacological Reviews 63 (2): 269–90. June 2011. doi:10.1124/pr.110.003301. PMID 21454438.
- ↑ 4.0 4.1 "Hydroxycarboxylic acid receptors". International Union of Basic and Clinical Pharmacology. http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=48.
- ↑ "Whole grain metabolite 3,5-dihydroxybenzoic acid is a beneficial nutritional molecule with the feature of a double-edged sword in human health: a critical review and dietary considerations". Critical Reviews in Food Science and Nutrition: 1–19. April 2023. doi:10.1080/10408398.2023.2203762. PMID 37096487.
- ↑ "Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81". The Journal of Biological Chemistry 284 (5): 2811–22. January 2009. doi:10.1074/jbc.M806409200. PMID 19047060.
- ↑ "Role of GPR81 in lactate-mediated reduction of adipose lipolysis". Biochemical and Biophysical Research Communications 377 (3): 987–91. December 2008. doi:10.1016/j.bbrc.2008.10.088. PMID 18952058.
- ↑ "History and Function of the Lactate Receptor GPR81/HCAR1 in the Brain: A Putative Therapeutic Target for the Treatment of Cerebral Ischemia". Neuroscience 526: 144–163. June 2023. doi:10.1016/j.neuroscience.2023.06.022. PMID 37391123.
Further reading
- "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters 520 (1–3): 97–101. June 2002. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878.
- "T lymphocyte activation gene identification by coregulated expression on DNA microarrays". Genomics 83 (6): 989–99. June 2004. doi:10.1016/j.ygeno.2003.12.019. PMID 15177553.
- "Lactate produced during labor modulates uterine inflammation via GPR81 (HCA1)". American Journal of Obstetrics and Gynecology 216 (1): 60.e1–60.e17. September 2016. doi:10.1016/j.ajog.2016.09.072. PMID 27615440.
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